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Merck
모든 사진(1)

주요 문서

SML2732

Sigma-Aldrich

DO34

≥98% (HPLC)

동의어(들):

(2-Benzyl-4-{[(2-methyl-2-propanyl)oxy]carbonyl}piperazinyl){4-[(4-trifluoromethoxy)phenyl]-1H-1,2,3-triazol-1-yl}methanone, 3-(Phenylmethyl)-4-[[4-[4-(trifluoromethoxy)phenyl]-1H-1,2,3-triazol-1-yl]carbonyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester

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About This Item

실험식(Hill 표기법):
C26H28F3N5O4
CAS Number:
Molecular Weight:
531.53
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

−20°C

SMILES string

O=C(N1CCN(CC1CC2=CC=CC=C2)C(OC(C)(C)C)=O)N3N=NC(C4=CC=C(C=C4)OC(F)(F)F)=C3

InChI

1S/C26H28F3N5O4/c1-25(2,3)38-24(36)32-13-14-33(20(16-32)15-18-7-5-4-6-8-18)23(35)34-17-22(30-31-34)19-9-11-21(12-10-19)37-26(27,28)29/h4-12,17,20H,13-16H2,1-3H3

InChI key

CQGMWUWJVBKTRM-UHFFFAOYSA-N

생화학적/생리학적 작용

Brain-penetrant, selective and highly potent diacylglycerol lipase (DAGLα/β, DAGLalpha & DAGLbeta) inhibitor in vitro and in vivo.
DO34 is a brain-penetrant, selective and highly potent diacylglycerol lipase inhibitor (recom human DAGLα/β pIC50 = 8.2/8.1 by SAG hydrolysis; mouse brain DAGLα/β pIC50 = 9.1-9.3/8.6 by ABPP ReDiMe) with detectable off-target activity toward only ABHD6 & PLA2G7 among all mouse brain serine hydrolases and little affinity toward cannabinoid receptors CB1/2. DO34 blocks depolarization-induced suppression of excitation (DSE IC50 = 0.18 μM) and inhibition (100% DSI blockage at 1 μM) in mouse cerebellar and hippocampal slices ex vivo, and attenuate LPS-induced neuroinflammatory responses by lowering brain 2-AG & PGE2 level in mice in vivo (50 mg/kg, i.p).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

Lot/Batch Number

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Carol A Gianessi et al.
Addiction biology, 25(3), e12768-e12768 (2019-05-06)
Individuals with alcohol use disorder exhibit compulsive habitual behaviors that are thought to be, in part, a consequence of chronic and persistent use of alcohol. The endocannabinoid system plays a critical role in habit learning and in ethanol self-administration, but
Xiaojie Liu et al.
Scientific reports, 6, 35829-35829 (2016-10-25)
The endocannabinoid 2-arachidonoylglycerol (2-AG) mediates retrograde synaptic depression including depolarization-induced suppression of excitation (DSE) and inhibition (DSI). 2-AG is degraded primarily by monoacylglycerol lipase (MAGL), which is expressed in neurons and astrocytes. Using knockout mice in which MAGL is deleted
Lesley D Schurman et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 39(30), 5949-5965 (2019-05-28)
Diacylglycerol lipase-α (DAGL-α), the principal biosynthetic enzyme of the endogenous cannabinoid 2-arachidonylglycerol (2-AG) on neurons, plays a key role in CB1 receptor-mediated synaptic plasticity and hippocampal neurogenesis, but its contribution to global hippocampal-mediated processes remains unknown. Thus, the present study

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